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Contributor Information

  • Name Laurent Rigoreau
  • Institute Newcastle University

Tool Details

  • Tool name: Dual DNA-PK/PI3K inhibitor KU-0060648 Small Molecule (Tool Compound)
  • Molecular formula: C33H34N4O4S
  • Tool type: Small molecules
  • Tool sub-type: Inhibitor
  • Purpose: Inhibitor
  • Description: KU-0060648 is a dual PI3-K and DNA-PK inhibitor (IC50 values are <0.1, 0.5, 4 and 19 nM for PI 3-Kd, PI 3-K?, PI 3-Ka and DNA-PK respectively). It inhibits proliferation of MCF7 cells in vitro and delays growth of MCF7 xenografts in mice. KU-0060648 can also enhance CRISP-Cas9-mediated homology-directed repair (HDR) efficiency, and attenuate nonhomologous end-joining (NHEJ).
  • Research area: Cancer ; Cell Cycle

  • For Research Use Only

Target Details

  • Target: Dual PI 3-K and DNA-PK inhibitor

Application Details

Handling

  • Purity: 582.71 g/mol
  • Solubility: Soluble to 100 mM in 2eq.HCl
  • Storage conditions: Store at -20°C
  • Shipping conditions: Dry Ice

Documentation

  • Available on request

References

  •   Robert et al. 2015. Genome Med. 7(1):93. PMID: 26307031.
  •   Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing.
  •   Munck et al. 2012. Mol Cancer Ther. 11(8):1789-98. PMID: 22576130.
  •   Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K.